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The 3rd Codeine and CWE megathread is here.
Credit to Mr Blonde for the following post, taken from the first page of the last codeine megathread. I have updated the paracetamol and ibuprofen solubility section.
In Australia codeine is commonly available over the counter in preparations where it is combined with paracetamol, ibuprofen and sometimes an antihistamine or decongestant. Codeine is also used recreationally, and it is the intent of this thread to inform users of the risks associated with the use of codeine and to describe preparation methods that may reduce some of these risks.
What is codeine?
Codeine is an opium alkaloid, found in plants of the papaver, primarily P. somniferum1. Structurally, it is very similar to morphine with the only difference being a methoxy moiety (R-O-CH3) attached at the 3 position on the molecule. When codeine is consumed by humans a portion of the dose is metabolized into morphine, which is carried out by the isoenzyme CYP2D62. Codeine is also metabolized into codeine-6-glucuronide via conjugation with glucuronic acid and n-demethylated to codeine. Some studies suggest that codeine-6-glucuronide may be responsible for part of the analgesia codeine provides3.
The effects of codeine are very similar to morphine, though less potent; only around 10% of the codeine is converted into morphine, and around 10% of the Caucasian population is deficient in the isoenzyme that is necessary for this conversion to take place4. Poor CYP2D6 metabolizers experience decreased levels of analgesia and euphoria compared to normal and extensive metabolizers. Anecdotal reports suggest that some users reach a 'ceiling dose' with codeine, usually around 400-600mg, and increasing the dose past this point does not increase euphoria or analgesia but rather leads to increased side effects. On the other hand, there are reports from users with a tolerance dosing as high as 2000mg or more.
Codeine effects, risks, interactions, routes of administration
The majority of the effects codeine has on the body are due to its partial metabolism to morphine in vivo. Thus, the effect profile of codeine is near identical to that of morphine. It causes feelings of euphoria, relaxation, sedation, analgesia, central nervous system and respiratory depression, pruritis (itchiness), nausea and constipation. Codeine itself is a potent histamine releaser5, and in high doses can cause a severe histamine response that includes severe itching and nausea, redness of the skin and some swelling (edema), similar to an allergic reaction.
Like with most other drugs, and all opioids, regular use of codeine can lead to tolerance, i.e. a higher dose is required for the same effect previously experienced on a lower dose. This can lead to addiction, although it is generally accepted in the medical community that because codeine is a less potent opiate this risk is less than with stronger substances6.
Codeine can be administered orally, intrarectally and intramuscular via injection. It is NOT safe to use the product of a cold water extraction for any type of injection, and it is NOT safe to use codeine via the intravenous route due to the large histamine response it causes. IV use can lead to pulmonary edema (fluid in the lungs) and can be potentially fatal. IV use has also been associated with seizures7, hypotension8, hypocalcaemia and decreased cardiac efficiency9. Intranasal and inhalation of codeine are ineffective methods of administration as the drug needs to go through first pass metabolism to morphine before it takes effect10; hence it would appear that oral use is the most efficient and safe method to use codeine.
As with most opioids, using codeine alongside other CNS depressants such as alcohol, benzodiazepines, barbiturates, GHB, other opioids, etc, can be dangerous due to the risk of overt CNS and respiratory depression. Although codeine is a relatively weak opioid and has a possible ceiling effect in most users, there is still significant risk of overdose, and care should be taken if it is to be combined with other CNS depressants. If such a combination is to be used, then doses of all substances should be lowered and administration should always be conducted carefully and slowly; start with a smaller dose and gradually increase until the desired effect is obtained.
Cold Water Extraction
A Cold Water Extraction (CWE) is a method by which codeine can be separated from some of the ingredients present in common OTC medications. When consumed in high doses, paracetamol and ibuprofen can cause severe physiological damage with a possibility of death(see Health Problems). If you have any allergies to these drugs, or intend to take more than the maximum prescribed/recommended dosages, it is in your best interests to remove the codeine from these preparations before use. Note however, that concentrating any addictive drug for the purposes of increasing dosage also increases the risk of dependence. The CWE procedure is very simple, although there are many variations. This thread will provide a couple of methods that have been used widely without problems.
Mr Blonde's CWE: 1) If using Nurofen + or a similarly hard tablet, they may be ground in a coffee grinder; most other codeine combo meds dissolve quite quickly by themselves i.e. just drop into a glass of cool water. The least amount of water possible should be used; 50mL for 24 tablets of 10mg codeine/500mg APAP or more will work. For preparations known to be more ‘sludgy’ (e.g. N+, certain codeine/APAP brands), the amount of water used can be increased. At most only 150-200mL of water should be used.
2) Once the tablets are dissolved, stir them and then place your filter over a cup. Coffee filters or lab filters may be used, but do take time to let the solution through. A shirt made of fabric that isn't too thin can be used also. The filter should be made damp with water, as this allows the solution to pass through easier.
3) Pour the solution through the filter, and wait until the stream of filtered solution slows to droplets. The filter may then be squeezed to extract any remaining liquid. NOTE: If you have use a shirt or other fabric as your filter, it is advisable to then filter the solution through coffee filters to ensure there is little to no paracetamol/ibuprofen in the solution.
4) That’s it! Dispose of the liquid by drinking, and dispose of the filtrate (paracetamol/ibuprofen) in your bin. Some users also do a second extraction on the paracetamol/ibuprofen left behind.
Erowid's CWE: The Procedure
1. Obtain a quantity of tablets containing codeine, check to see if they contain anything other than codeine, caffeine, acetaminophen or aspirin. If they do, and you don't know whether or not it will be a problem, your best bet is not to use them. Measure out your desired amount of codeine (ex. 64 mg = 8 tablets * 8mg/tablet). You may want to add 2 extra tablets as it is quite likely you will lose some codeine in the procedure. As you get more experience with the procedure you will be able to get approx. 95% of the codeine extracted.
2. Measure out some nice hot water, use approx. 40ml / 20 tablets or more if needed. I would suggest you don't go over 50ml for 20 tablets. I don't know if the use of boiling water would destroy any of the codeine but your best bet is not to use it. Use hot water but not boiling. Make sure the tablets dissolve completely. Some dissolve on contact with water while others need some help dissolving by crushing them. Note : not all of the tablet will dissolve, there are water-insoluble fillers in the tablet and not all of the A/A will dissolve either(which is what we want).
[Most sources recommend that codeine not be stored at temperatures in excess of 40C (104F), so its probably better to use warm, but not hot, water. I find that it is best to crash the tablets completely in a container, and then dissolve them in a glass with water.]
3. Place the solution in a cold bath, I just use some ice cubes in a container of water. Stir the mixture occasionally until the solution drops to about 15C or lower. You won't need a thermometer to measure the temperature, just make sure it's "cold". This will take about 30 min. If you wish to speed this up, you can use less water to dissolve the tablets, and add ice chips to cool the mixture faster. Just make sure you don't add so much ice that you drastically increase the volume of the mixture.
4. Filter the solution using whatever you have. Coffee filters work well, but lab filters work the best. Just make sure you don't end up with obvious solids in the filtered solution. This will take about 1 hr. You may also want to rinse the solids left over in the filter with some ice-water to extract any remaining codeine.
[With aspirin this will take only about 20-30 minutes.]
5. Drink and enjoy! The solution will be _very_ bitter, so I mix a little Kool-aid powder into the solution. The taste isn't really bad but it's similar to sucking on a lemon.
[One gets used to the taste after a while.]
6. Sit back and wait for the effects. Because the codeine is already in solution it only needs to be absorbed, while codeine in the tablet form must dissolve before being absorbed. Because of this, the effects will probably become noticeable within 15min.
Note : Evaporating the mixture if so desired should be done slowly and under low heat; at 80°C codeine will be destroyed. Evaporating the mixture under a fan or in the oven on low heat with the door open is suggested, though it will take a while to completely evaporate.
It is important to note that some available codeine containing medications also include phenylephrine, pseudoephedrine, doxylamine succinate or other active ingredients. These are often not suitable for a CWE as they may also be soluble in water and when consumed in high doses are potentially dangerous. Although doxylamine succinate has been used synergistically with codeine, it can be dangerous to consume a high dose of it and should best be obtained separately from the codeine as it will not be removed during the CWE process.
Commonly Made Mistakes During CWE
Dumping the solution straight into a coffee filter- Coffee filters can be fragile, and will also clog up easily. It is probably best to filter using another material first (e.g. shirt), then to pour the filtrate through a coffee filter. The filter should be folded as shown on this website: http://www.dynamicscience.com.au/tes...ngfilterpr.htm
Forgetting to Wet the Filters - Whether a shirt or proper filter is used, both are absorbent and will soak up some of the solution resulting in loss of the final product. To avoid this, the filter should be soaked with water before pouring through the mixture; this allows the solution to pass through quicker and easier and also minimizes loss of product.
Putting the Solution Through a Shirt then Neglecting Coffee Filters - Although many users simply use a shirt or other fabric as their filter, it is highly advisable to use coffee filters or lab filters. Some shirts are made of quite thin and porous material which may let through enough paracetamol or ibuprofen to cause problems. Proper lab filters can be obtained online or from chemical suppliers easily and without suspicion.
Too Much Water on the Second Wash - If a second wash is performed then the amount of paracetamol or ibuprofen being ingested will be increased. If codeine is being consumed long term in this fashion, then the increased intake of these substances may lead to health problems. Below is a table showing the solubility of the ingredients commonly found in OTC codeine preparations.
Solubility of ibuprofen and paracetamol
These figures should be taken as approximates only. Don't forget this only includes how much para/ibu is dissolved, and does not include suspended solid particles of paracetamol and ibuprofen. The purpose of filtering is to remove as many of these solid particles as possible. If filtering is not done properly, toxic levels of paracetamol or ibuprofen can remain in your final product.
Solubility of Ibuprofen
The solubility of ibuprofen in water at 25 degrees celcius or lower is less is than 1mg per ml. Source.
At 31 degrees 100mg dissolves in 100 ml (1mg/ml).
At 21 degrees, 7.8mg dissolves in 100ml (0.078mg/ml)
Solubility of Paracetamol
Mg paracetamol dissolved in ml of water at degrees celcius. Source.
0 - 7.21mg/ml
5 - 8.21mg/ml
10 - 9.44mg/ml
15 - 10.97mg/ml
20 - 12.78mg/ml
25 - 14.90mg/ml
Having a Coffee Filter Break and NOT Re-filtering - Pouring liquid too quickly into a coffee filter can lead to breakage of the filter itself. It is important to note when this has happened, as consuming a CWE that has not been filtered correctly could be harmful or fatal. Squeezing a coffee filter can increase the chances of it breaking. Occasionally the hole in the filter will be large and noticeable, but sometimes can be small and easy to miss at first glance. A sign of a broken filter is the liquid pouring through at a quicker rate then expected. If this happens, then you must re-filter the solution. Using two coffee filters, one place inside the other, can reduce the chances of this happening.
General Hastiness - CWE can be a bit of a time consuming process and as a result, it is easy to want to take shortcuts however, it is very unwise to do so. Let your solution filter in its own time; if you did everything right it will do it on its own. If in doubt about a solutions safety, due to seeming extremely cloudy, suspecting a hole in your filter, etc. REFILTER! Do not tell yourself it will be fine and gulp it down anyway, wait the extra time to re-filter and know you are safe.
Less Common Mistakes Made During CWE
Squeezing of Coffee Filters - Sometimes it can take quite a while for your solution to pass through a coffee filter, it can feel like a lifetime, however it is important not to let oneself get impatient and attempt to squeeze or push their solution through the coffee filters to speed up the process. Anecdotally, users have reported feeling ill (nausea, stomach pain, etc...) after not filtering correctly. Do NOT do this; it is not worth neither risking your health or your life to save a small wait to consume codeine. Just think the longer since you ate the harder it will hit, so a few extra minutes waiting won’t kill you, as it turns out being impatient just might.
Tipping Solution Out of Coffee Filters - At least one user has reported that after waiting for filtering to occur (coffee filter), he became impatient and removed the filter and poured the solution out of that into the solution for consumption. He reported extreme nausea and vomiting as a result. Let it filter properly, and if you aren't patient enough for this method use the shirt filter with a coffee filter afterward.
IV Use of Codeine - POTENTIALLY FATAL - DO NOT ATTEMPT THIS. This is far from common, but it is not unheard of. It is extremely unsafe as it puts you at risk of pulmonary edema (fluid in the lungs) among other various life-threatening complications from such a strong histamine reaction. See the above section on Codeine effects and risks, and also see these links: 7, 8, 9.
Law and Scheduling
As of May 1, 2010, all over the counter preparations of codeine were moved into the Schedule III category, making them Pharmacist Only Medicines11. Many pharmacies now require identification when purchasing these products. In addition to this, the size of packs has been reduced to a maximum of a five day supply (40 Panadeine, 30 Nurofen Plus). Panadeine Extra, containing 15mg of codeine a tablet, is restricted to a maximum of a 24 pack size. This change was in response to media reports of codeine abuse and was put forward by the Therapeutic Goods Administration, the federal body that oversees the scheduling and sale of medications and poisons in Australia. Interestingly, the Pharmaceutical Guild of Australia has made comments that were critical of this change in the laws, claiming that it will do little to reduce abuse and inconvenience the majority of people who do not abuse the medication11.
There are also codeine products containing up to 30mg of codeine in combination with paracetamol, which are Schedule IV and require a prescription to possess.
Codeine by itself with no combination product is Schedule VIII, requiring a prescription to possess and being subject to strict state based laws regarding Drugs of Dependence.
Underestimating Codeine’s Abuse Potential
Although codeine is considered a 'weak' opioid with limitations to it's use, there is potential for addiction. Media stories prior to the rescheduling of codeine highlighted that there were addicts swallowing the tablets whole to obtain the codeine, and in in the process causing liver, kidney and gastrointestinal damage amongst other problems. Whilst a CWE avoids these issues, it can lead to an increase in use and tolerance. Users should keep in mind that codeine can be habit forming, and that constant use with abrupt cessation can lead to minor to moderate withdrawal symptoms.
Health Problems
There are a variety of health problems that are associated with codeine product use and abuse, either caused by the combination ingredients or by the codeine itself.
Paracetamol: This is a potentially deadly substance to overdose on. Normally, paracetamol is metabolized by the liver into harmless by-products; however, when too much paracetamol is consumed the liver is forced to resort to a metabolic pathway that produces the toxic metabolite n-acetyl-p-benzoquinoneimine (NAPQI). When paracetamol is consumed in usual doses, a small amount of NAPQI is normally produced and then conjugated by the liver rendering it harmless. When large amounts of paracetamol are taken, or if a large amount is taken over a period of time, the liver is overloaded and produces more and more NAPQI which it is then unable to conjugate. If not treated in time this can lead to liver damage, multiple organ failure and death.
According to the Medical Journal of Australia's 'Guidelines for the management of paracetamol poisoning in Australia and New Zealand', a dose of paracetamol that 'may be associated with hepatic injury' includes 200mg/kg or 10 grams (whichever is less) over a period of less then 8 hours, or if used chronically, as low as 100mg/kg or 4 grams a day (whichever is less) in patients with risk factors such as heavy alcohol use, dehydration, fasting or co-ingestion of enzyme inducing substances.
It is highly recommended that people using paracetamol or doing a CWE on codeine-paracetamol products keep N-acetylcysteine, an antidote, on hand in case of overdose. Although this is no replacement for medical assistance, it can help your liver to conjugate the NAPQI by acting as a precursor for the conjugant glutathione, and keeping it on hand may very well save you in the case of an accidental overdose.
IMPORTANT: IF YOU BELIEVE YOU HAVE TAKEN AN OVERDOSE OF PARACETAMOL, YOU SHOULD URGENTLY SEEK MEDICAL ADVICE AND TREATMENT. THERE IS AN ANTIDOTE AVAILABLE, HOWEVER OFTEN TIMES SYMPTOMS OF AN OVERDOSE DO NOT PRESENT FOR UP TO SEVERAL DAYS DURING WHICH TIME SEVERE LIVER DAMAGE CAN OCCUR.
Ibuprofen: A severe overdose of ibuprofen can be life threatening or at the very least cause a good deal of damage to your body, so if you suspect you may have overdosed on ibuprofen it is important to seek medical attention. Symptoms of an ibuprofen overdose include stomach ulcers, nausea, headaches, dizziness, drowsiness, tinnitus, bleeding in the gastrointestinal tract, seizures, hypotension, tachycardia, liver dysfunction, kidney failure, respiratory depression and cardiac arrest13. Please see reference 12 for more info on ibuprofen overdose.
There is also evidence to suggest Ibuprofen is not suitable for human consumption in the long term. Long term use of ibuprofen has been associated with stomach ulcers which can bleed and rupture, diarrhea or constipation, priapism, hypertension and hearing loss. It has also been linked to increases in stroke and heart attack, even at or below the recommended dose.16.
Aspirin: Aspirin in combination with codeine is relatively rare in Australia; it can sometimes be found in prescription medications or OTC. Although aspirin can be removed via a CWE, there have been reports of effervescent tablets which will disperse into solution and are not suitable for a CWE.
An aspirin overdose can cause nausea, abdominal pain, tinnitus, hyperventilation, metabolic acidosis, low potassium and glucose levels, neurological effects such as hallucinations and agitation, pulmonary and cerebral edema and seizures. A dose greater then 150mg/kg of body weight can produce toxic effects, and long term use has been associated with tinnitus and stomach ulcers14.
A suspected overdose should, of course, warrant medical attention.
BIBLIOGRAPHY
1. Valva V La, Sabato, Sergio and Siniscalco Gigliano G. Morphology and Alkaloid Chemistry of Papaver setigerum DC. (Papaveraceae). Taxon. 1985;34(2):6.
2. Meyer MR, Maurer HH. Absorption, distribution, metabolism and excretion pharmacogenomics of drugs of abuse. Pharmacogenomics. 2011;12(2):215-33. Available at: http://www.ncbi.nlm.nih.gov/pubmed/21332315 [Accessed July 6, 2011].
3. Srinivasan V, Wielbo D, Simpkins J, et al. Analgesic and immunomodulatory effects of codeine and codeine 6-glucuronide. Pharmaceutical research. 1996;13(2):296-300. Available at: http://www.ncbi.nlm.nih.gov/pubmed/8932452 [Accessed August 8, 2011].
4. Leon J de, Susce MT, Pan R-M, et al. The CYP2D6 poor metabolizer phenotype may be associated with risperidone adverse drug reactions and discontinuation. The Journal of clinical psychiatry. 2005;66(1):15-27. Available at: http://www.ncbi.nlm.nih.gov/pubmed/15669884.
5. Perzanowska M, Malhotra D, Skinner SP, et al. The effect of cetirizine and loratadine on codeine-induced histamine release in human skin in vivo assessed by cutaneous microdialysis. Inflammation Research. 1996;45(9):486-490. Available at: http://www.springerlink.com/index/10.1007/BF02252321 [Accessed August 8, 2011].
6. Eddy NB, Friebel H, Hahn KJ, Halbach H. Codeine and its alternates for pain and cough relief. 5. Discussion and summary. Bulletin of the World Health Organization. 1969;40(5):721-30. Available at: http://www.pubmedcentral.nih.gov/art...rtype=abstract.
7. Zolezzi M, Al Mohaimeed SA. Seizures with Intravenous Codeine Phosphate. The Annals of Pharmacotherapy. 2001;35:1211-1213. Available at: http://www.theannals.com/cgi/doi/10.1345/aph.10326 [Accessed August 8, 2011].
8. PARKE TJ, NANDI PR, BIRD KJ, JEWKES DA. Profound hypotension following intravenous codeine phosphate. Anaesthesia. 1992;47(10):852-854. Available at: http://doi.wiley.com/10.1111/j.1365-2044.1992.tb03145.x [Accessed August 8, 2011].
9. Brown K, Halperin LF, Malhotra A, et al. Hypocalcaemia and a low cardiac output after intravenous codeine phosphate injection: need for an additional mechanism to remove ionized calcium. NDT Plus. 2009;2(5):401-404. Available at: http://ndtplus.oxfordjournals.org/cg...ndtplus/sfp054 [Accessed August 8, 2011].
10. Poulsen L, Brøsen K, Arendt-Nielsen L, et al. Codeine and morphine in extensive and poor metabolizers of sparteine: pharmacokinetics, analgesic effect and side effects. European Journal of Clinical Pharmacology. 1996;51(3-4):289-295. Available at: http://www.springerlink.com/openurl..../s002280050200 [Accessed August 8, 2011].
11. Simmons A. Codeine crackdown comes into effect. ABC NEWS. 2010:1. Available at: http://www.abc.net.au/news/2010-05-0...-effect/417324.
12. McElwee NE, Veltri JC, Bradford DC, Rollins DE. A prospective, population-based study of acute ibuprofen overdose: complications are rare and routine serum levels not warranted. Annals of emergency medicine. 1990;19(6):657-62. Available at: http://www.ncbi.nlm.nih.gov/pubmed/2188537 [Accessed August 12, 2011].
13. Vale JA, Meredith TJ. Acute poisoning due to non-steroidal anti-inflammatory drugs. Clinical features and management. Medical toxicology. 1(1):12-31. Available at: http://www.ncbi.nlm.nih.gov/pubmed/3537613 [Accessed August 12, 2011].
14. Thisted B, Krantz T, Strøom J, Sørensen MB. Acute salicylate self-poisoning in 177 consecutive patients treated in ICU. Acta anaesthesiologica Scandinavica. 1987;31(4):312-6. Available at: http://www.ncbi.nlm.nih.gov/pubmed/3591255 [Accessed August 12, 2011].
15. : Eric Perez, MD, Department of Emergency Medicine, St. Luke’s-Roosevelt Hospital Center, New York, NY. Review provided by VeriMed Healthcare Network. Also reviewed by David Zieve, MD, MHA, Medical Director, A.D.A.M. I. Opiate withdrawal. Medline Plus. 2011:1. Available at: http://www.nlm.nih.gov/medlineplus/e...cle/000949.htm.
16. Cause-Specific Cardiovascular Risk Associated With Nonsteroidal Antiinflammatory Drugs Among Healthy Individuals
Credit to Mr Blonde for the following post, taken from the first page of the last codeine megathread. I have updated the paracetamol and ibuprofen solubility section.
In Australia codeine is commonly available over the counter in preparations where it is combined with paracetamol, ibuprofen and sometimes an antihistamine or decongestant. Codeine is also used recreationally, and it is the intent of this thread to inform users of the risks associated with the use of codeine and to describe preparation methods that may reduce some of these risks.
What is codeine?
Codeine is an opium alkaloid, found in plants of the papaver, primarily P. somniferum1. Structurally, it is very similar to morphine with the only difference being a methoxy moiety (R-O-CH3) attached at the 3 position on the molecule. When codeine is consumed by humans a portion of the dose is metabolized into morphine, which is carried out by the isoenzyme CYP2D62. Codeine is also metabolized into codeine-6-glucuronide via conjugation with glucuronic acid and n-demethylated to codeine. Some studies suggest that codeine-6-glucuronide may be responsible for part of the analgesia codeine provides3.
The effects of codeine are very similar to morphine, though less potent; only around 10% of the codeine is converted into morphine, and around 10% of the Caucasian population is deficient in the isoenzyme that is necessary for this conversion to take place4. Poor CYP2D6 metabolizers experience decreased levels of analgesia and euphoria compared to normal and extensive metabolizers. Anecdotal reports suggest that some users reach a 'ceiling dose' with codeine, usually around 400-600mg, and increasing the dose past this point does not increase euphoria or analgesia but rather leads to increased side effects. On the other hand, there are reports from users with a tolerance dosing as high as 2000mg or more.
Codeine effects, risks, interactions, routes of administration
The majority of the effects codeine has on the body are due to its partial metabolism to morphine in vivo. Thus, the effect profile of codeine is near identical to that of morphine. It causes feelings of euphoria, relaxation, sedation, analgesia, central nervous system and respiratory depression, pruritis (itchiness), nausea and constipation. Codeine itself is a potent histamine releaser5, and in high doses can cause a severe histamine response that includes severe itching and nausea, redness of the skin and some swelling (edema), similar to an allergic reaction.
Like with most other drugs, and all opioids, regular use of codeine can lead to tolerance, i.e. a higher dose is required for the same effect previously experienced on a lower dose. This can lead to addiction, although it is generally accepted in the medical community that because codeine is a less potent opiate this risk is less than with stronger substances6.
Codeine can be administered orally, intrarectally and intramuscular via injection. It is NOT safe to use the product of a cold water extraction for any type of injection, and it is NOT safe to use codeine via the intravenous route due to the large histamine response it causes. IV use can lead to pulmonary edema (fluid in the lungs) and can be potentially fatal. IV use has also been associated with seizures7, hypotension8, hypocalcaemia and decreased cardiac efficiency9. Intranasal and inhalation of codeine are ineffective methods of administration as the drug needs to go through first pass metabolism to morphine before it takes effect10; hence it would appear that oral use is the most efficient and safe method to use codeine.
As with most opioids, using codeine alongside other CNS depressants such as alcohol, benzodiazepines, barbiturates, GHB, other opioids, etc, can be dangerous due to the risk of overt CNS and respiratory depression. Although codeine is a relatively weak opioid and has a possible ceiling effect in most users, there is still significant risk of overdose, and care should be taken if it is to be combined with other CNS depressants. If such a combination is to be used, then doses of all substances should be lowered and administration should always be conducted carefully and slowly; start with a smaller dose and gradually increase until the desired effect is obtained.
Cold Water Extraction
A Cold Water Extraction (CWE) is a method by which codeine can be separated from some of the ingredients present in common OTC medications. When consumed in high doses, paracetamol and ibuprofen can cause severe physiological damage with a possibility of death(see Health Problems). If you have any allergies to these drugs, or intend to take more than the maximum prescribed/recommended dosages, it is in your best interests to remove the codeine from these preparations before use. Note however, that concentrating any addictive drug for the purposes of increasing dosage also increases the risk of dependence. The CWE procedure is very simple, although there are many variations. This thread will provide a couple of methods that have been used widely without problems.
Mr Blonde's CWE: 1) If using Nurofen + or a similarly hard tablet, they may be ground in a coffee grinder; most other codeine combo meds dissolve quite quickly by themselves i.e. just drop into a glass of cool water. The least amount of water possible should be used; 50mL for 24 tablets of 10mg codeine/500mg APAP or more will work. For preparations known to be more ‘sludgy’ (e.g. N+, certain codeine/APAP brands), the amount of water used can be increased. At most only 150-200mL of water should be used.
2) Once the tablets are dissolved, stir them and then place your filter over a cup. Coffee filters or lab filters may be used, but do take time to let the solution through. A shirt made of fabric that isn't too thin can be used also. The filter should be made damp with water, as this allows the solution to pass through easier.
3) Pour the solution through the filter, and wait until the stream of filtered solution slows to droplets. The filter may then be squeezed to extract any remaining liquid. NOTE: If you have use a shirt or other fabric as your filter, it is advisable to then filter the solution through coffee filters to ensure there is little to no paracetamol/ibuprofen in the solution.
4) That’s it! Dispose of the liquid by drinking, and dispose of the filtrate (paracetamol/ibuprofen) in your bin. Some users also do a second extraction on the paracetamol/ibuprofen left behind.
Erowid's CWE: The Procedure
1. Obtain a quantity of tablets containing codeine, check to see if they contain anything other than codeine, caffeine, acetaminophen or aspirin. If they do, and you don't know whether or not it will be a problem, your best bet is not to use them. Measure out your desired amount of codeine (ex. 64 mg = 8 tablets * 8mg/tablet). You may want to add 2 extra tablets as it is quite likely you will lose some codeine in the procedure. As you get more experience with the procedure you will be able to get approx. 95% of the codeine extracted.
2. Measure out some nice hot water, use approx. 40ml / 20 tablets or more if needed. I would suggest you don't go over 50ml for 20 tablets. I don't know if the use of boiling water would destroy any of the codeine but your best bet is not to use it. Use hot water but not boiling. Make sure the tablets dissolve completely. Some dissolve on contact with water while others need some help dissolving by crushing them. Note : not all of the tablet will dissolve, there are water-insoluble fillers in the tablet and not all of the A/A will dissolve either(which is what we want).
[Most sources recommend that codeine not be stored at temperatures in excess of 40C (104F), so its probably better to use warm, but not hot, water. I find that it is best to crash the tablets completely in a container, and then dissolve them in a glass with water.]
3. Place the solution in a cold bath, I just use some ice cubes in a container of water. Stir the mixture occasionally until the solution drops to about 15C or lower. You won't need a thermometer to measure the temperature, just make sure it's "cold". This will take about 30 min. If you wish to speed this up, you can use less water to dissolve the tablets, and add ice chips to cool the mixture faster. Just make sure you don't add so much ice that you drastically increase the volume of the mixture.
4. Filter the solution using whatever you have. Coffee filters work well, but lab filters work the best. Just make sure you don't end up with obvious solids in the filtered solution. This will take about 1 hr. You may also want to rinse the solids left over in the filter with some ice-water to extract any remaining codeine.
[With aspirin this will take only about 20-30 minutes.]
5. Drink and enjoy! The solution will be _very_ bitter, so I mix a little Kool-aid powder into the solution. The taste isn't really bad but it's similar to sucking on a lemon.
[One gets used to the taste after a while.]
6. Sit back and wait for the effects. Because the codeine is already in solution it only needs to be absorbed, while codeine in the tablet form must dissolve before being absorbed. Because of this, the effects will probably become noticeable within 15min.
Note : Evaporating the mixture if so desired should be done slowly and under low heat; at 80°C codeine will be destroyed. Evaporating the mixture under a fan or in the oven on low heat with the door open is suggested, though it will take a while to completely evaporate.
It is important to note that some available codeine containing medications also include phenylephrine, pseudoephedrine, doxylamine succinate or other active ingredients. These are often not suitable for a CWE as they may also be soluble in water and when consumed in high doses are potentially dangerous. Although doxylamine succinate has been used synergistically with codeine, it can be dangerous to consume a high dose of it and should best be obtained separately from the codeine as it will not be removed during the CWE process.
Commonly Made Mistakes During CWE
Dumping the solution straight into a coffee filter- Coffee filters can be fragile, and will also clog up easily. It is probably best to filter using another material first (e.g. shirt), then to pour the filtrate through a coffee filter. The filter should be folded as shown on this website: http://www.dynamicscience.com.au/tes...ngfilterpr.htm
Forgetting to Wet the Filters - Whether a shirt or proper filter is used, both are absorbent and will soak up some of the solution resulting in loss of the final product. To avoid this, the filter should be soaked with water before pouring through the mixture; this allows the solution to pass through quicker and easier and also minimizes loss of product.
Putting the Solution Through a Shirt then Neglecting Coffee Filters - Although many users simply use a shirt or other fabric as their filter, it is highly advisable to use coffee filters or lab filters. Some shirts are made of quite thin and porous material which may let through enough paracetamol or ibuprofen to cause problems. Proper lab filters can be obtained online or from chemical suppliers easily and without suspicion.
Too Much Water on the Second Wash - If a second wash is performed then the amount of paracetamol or ibuprofen being ingested will be increased. If codeine is being consumed long term in this fashion, then the increased intake of these substances may lead to health problems. Below is a table showing the solubility of the ingredients commonly found in OTC codeine preparations.
Solubility of ibuprofen and paracetamol
These figures should be taken as approximates only. Don't forget this only includes how much para/ibu is dissolved, and does not include suspended solid particles of paracetamol and ibuprofen. The purpose of filtering is to remove as many of these solid particles as possible. If filtering is not done properly, toxic levels of paracetamol or ibuprofen can remain in your final product.
Solubility of Ibuprofen
The solubility of ibuprofen in water at 25 degrees celcius or lower is less is than 1mg per ml. Source.
At 31 degrees 100mg dissolves in 100 ml (1mg/ml).
At 21 degrees, 7.8mg dissolves in 100ml (0.078mg/ml)
Solubility of Paracetamol
Mg paracetamol dissolved in ml of water at degrees celcius. Source.
0 - 7.21mg/ml
5 - 8.21mg/ml
10 - 9.44mg/ml
15 - 10.97mg/ml
20 - 12.78mg/ml
25 - 14.90mg/ml
Having a Coffee Filter Break and NOT Re-filtering - Pouring liquid too quickly into a coffee filter can lead to breakage of the filter itself. It is important to note when this has happened, as consuming a CWE that has not been filtered correctly could be harmful or fatal. Squeezing a coffee filter can increase the chances of it breaking. Occasionally the hole in the filter will be large and noticeable, but sometimes can be small and easy to miss at first glance. A sign of a broken filter is the liquid pouring through at a quicker rate then expected. If this happens, then you must re-filter the solution. Using two coffee filters, one place inside the other, can reduce the chances of this happening.
General Hastiness - CWE can be a bit of a time consuming process and as a result, it is easy to want to take shortcuts however, it is very unwise to do so. Let your solution filter in its own time; if you did everything right it will do it on its own. If in doubt about a solutions safety, due to seeming extremely cloudy, suspecting a hole in your filter, etc. REFILTER! Do not tell yourself it will be fine and gulp it down anyway, wait the extra time to re-filter and know you are safe.
Less Common Mistakes Made During CWE
Squeezing of Coffee Filters - Sometimes it can take quite a while for your solution to pass through a coffee filter, it can feel like a lifetime, however it is important not to let oneself get impatient and attempt to squeeze or push their solution through the coffee filters to speed up the process. Anecdotally, users have reported feeling ill (nausea, stomach pain, etc...) after not filtering correctly. Do NOT do this; it is not worth neither risking your health or your life to save a small wait to consume codeine. Just think the longer since you ate the harder it will hit, so a few extra minutes waiting won’t kill you, as it turns out being impatient just might.
Tipping Solution Out of Coffee Filters - At least one user has reported that after waiting for filtering to occur (coffee filter), he became impatient and removed the filter and poured the solution out of that into the solution for consumption. He reported extreme nausea and vomiting as a result. Let it filter properly, and if you aren't patient enough for this method use the shirt filter with a coffee filter afterward.
IV Use of Codeine - POTENTIALLY FATAL - DO NOT ATTEMPT THIS. This is far from common, but it is not unheard of. It is extremely unsafe as it puts you at risk of pulmonary edema (fluid in the lungs) among other various life-threatening complications from such a strong histamine reaction. See the above section on Codeine effects and risks, and also see these links: 7, 8, 9.
Law and Scheduling
As of May 1, 2010, all over the counter preparations of codeine were moved into the Schedule III category, making them Pharmacist Only Medicines11. Many pharmacies now require identification when purchasing these products. In addition to this, the size of packs has been reduced to a maximum of a five day supply (40 Panadeine, 30 Nurofen Plus). Panadeine Extra, containing 15mg of codeine a tablet, is restricted to a maximum of a 24 pack size. This change was in response to media reports of codeine abuse and was put forward by the Therapeutic Goods Administration, the federal body that oversees the scheduling and sale of medications and poisons in Australia. Interestingly, the Pharmaceutical Guild of Australia has made comments that were critical of this change in the laws, claiming that it will do little to reduce abuse and inconvenience the majority of people who do not abuse the medication11.
There are also codeine products containing up to 30mg of codeine in combination with paracetamol, which are Schedule IV and require a prescription to possess.
Codeine by itself with no combination product is Schedule VIII, requiring a prescription to possess and being subject to strict state based laws regarding Drugs of Dependence.
Underestimating Codeine’s Abuse Potential
Although codeine is considered a 'weak' opioid with limitations to it's use, there is potential for addiction. Media stories prior to the rescheduling of codeine highlighted that there were addicts swallowing the tablets whole to obtain the codeine, and in in the process causing liver, kidney and gastrointestinal damage amongst other problems. Whilst a CWE avoids these issues, it can lead to an increase in use and tolerance. Users should keep in mind that codeine can be habit forming, and that constant use with abrupt cessation can lead to minor to moderate withdrawal symptoms.
Health Problems
There are a variety of health problems that are associated with codeine product use and abuse, either caused by the combination ingredients or by the codeine itself.
Paracetamol: This is a potentially deadly substance to overdose on. Normally, paracetamol is metabolized by the liver into harmless by-products; however, when too much paracetamol is consumed the liver is forced to resort to a metabolic pathway that produces the toxic metabolite n-acetyl-p-benzoquinoneimine (NAPQI). When paracetamol is consumed in usual doses, a small amount of NAPQI is normally produced and then conjugated by the liver rendering it harmless. When large amounts of paracetamol are taken, or if a large amount is taken over a period of time, the liver is overloaded and produces more and more NAPQI which it is then unable to conjugate. If not treated in time this can lead to liver damage, multiple organ failure and death.
According to the Medical Journal of Australia's 'Guidelines for the management of paracetamol poisoning in Australia and New Zealand', a dose of paracetamol that 'may be associated with hepatic injury' includes 200mg/kg or 10 grams (whichever is less) over a period of less then 8 hours, or if used chronically, as low as 100mg/kg or 4 grams a day (whichever is less) in patients with risk factors such as heavy alcohol use, dehydration, fasting or co-ingestion of enzyme inducing substances.
It is highly recommended that people using paracetamol or doing a CWE on codeine-paracetamol products keep N-acetylcysteine, an antidote, on hand in case of overdose. Although this is no replacement for medical assistance, it can help your liver to conjugate the NAPQI by acting as a precursor for the conjugant glutathione, and keeping it on hand may very well save you in the case of an accidental overdose.
IMPORTANT: IF YOU BELIEVE YOU HAVE TAKEN AN OVERDOSE OF PARACETAMOL, YOU SHOULD URGENTLY SEEK MEDICAL ADVICE AND TREATMENT. THERE IS AN ANTIDOTE AVAILABLE, HOWEVER OFTEN TIMES SYMPTOMS OF AN OVERDOSE DO NOT PRESENT FOR UP TO SEVERAL DAYS DURING WHICH TIME SEVERE LIVER DAMAGE CAN OCCUR.
Ibuprofen: A severe overdose of ibuprofen can be life threatening or at the very least cause a good deal of damage to your body, so if you suspect you may have overdosed on ibuprofen it is important to seek medical attention. Symptoms of an ibuprofen overdose include stomach ulcers, nausea, headaches, dizziness, drowsiness, tinnitus, bleeding in the gastrointestinal tract, seizures, hypotension, tachycardia, liver dysfunction, kidney failure, respiratory depression and cardiac arrest13. Please see reference 12 for more info on ibuprofen overdose.
There is also evidence to suggest Ibuprofen is not suitable for human consumption in the long term. Long term use of ibuprofen has been associated with stomach ulcers which can bleed and rupture, diarrhea or constipation, priapism, hypertension and hearing loss. It has also been linked to increases in stroke and heart attack, even at or below the recommended dose.16.
Aspirin: Aspirin in combination with codeine is relatively rare in Australia; it can sometimes be found in prescription medications or OTC. Although aspirin can be removed via a CWE, there have been reports of effervescent tablets which will disperse into solution and are not suitable for a CWE.
An aspirin overdose can cause nausea, abdominal pain, tinnitus, hyperventilation, metabolic acidosis, low potassium and glucose levels, neurological effects such as hallucinations and agitation, pulmonary and cerebral edema and seizures. A dose greater then 150mg/kg of body weight can produce toxic effects, and long term use has been associated with tinnitus and stomach ulcers14.
A suspected overdose should, of course, warrant medical attention.
BIBLIOGRAPHY
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7. Zolezzi M, Al Mohaimeed SA. Seizures with Intravenous Codeine Phosphate. The Annals of Pharmacotherapy. 2001;35:1211-1213. Available at: http://www.theannals.com/cgi/doi/10.1345/aph.10326 [Accessed August 8, 2011].
8. PARKE TJ, NANDI PR, BIRD KJ, JEWKES DA. Profound hypotension following intravenous codeine phosphate. Anaesthesia. 1992;47(10):852-854. Available at: http://doi.wiley.com/10.1111/j.1365-2044.1992.tb03145.x [Accessed August 8, 2011].
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11. Simmons A. Codeine crackdown comes into effect. ABC NEWS. 2010:1. Available at: http://www.abc.net.au/news/2010-05-0...-effect/417324.
12. McElwee NE, Veltri JC, Bradford DC, Rollins DE. A prospective, population-based study of acute ibuprofen overdose: complications are rare and routine serum levels not warranted. Annals of emergency medicine. 1990;19(6):657-62. Available at: http://www.ncbi.nlm.nih.gov/pubmed/2188537 [Accessed August 12, 2011].
13. Vale JA, Meredith TJ. Acute poisoning due to non-steroidal anti-inflammatory drugs. Clinical features and management. Medical toxicology. 1(1):12-31. Available at: http://www.ncbi.nlm.nih.gov/pubmed/3537613 [Accessed August 12, 2011].
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16. Cause-Specific Cardiovascular Risk Associated With Nonsteroidal Antiinflammatory Drugs Among Healthy Individuals
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